CN1784236A - 雄激素受体调节剂及其使用方法 - Google Patents

雄激素受体调节剂及其使用方法 Download PDF

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Publication number
CN1784236A
CN1784236A CNA2004800122535A CN200480012253A CN1784236A CN 1784236 A CN1784236 A CN 1784236A CN A2004800122535 A CNA2004800122535 A CN A2004800122535A CN 200480012253 A CN200480012253 A CN 200480012253A CN 1784236 A CN1784236 A CN 1784236A
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CN
China
Prior art keywords
methyl
alkyl
aza
androst
aryl
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Pending
Application number
CNA2004800122535A
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English (en)
Chinese (zh)
Inventor
R·S·梅斯纳
J·J·珀金斯
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
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Merck and Co Inc
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Publication of CN1784236A publication Critical patent/CN1784236A/zh
Pending legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26—Androgens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CNA2004800122535A 2003-05-07 2004-05-03 雄激素受体调节剂及其使用方法 Pending CN1784236A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US46857903P 2003-05-07 2003-05-07
US60/468,579 2003-05-07

Publications (1)

Publication Number Publication Date
CN1784236A true CN1784236A (zh) 2006-06-07

Family

ID=33452214

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA2004800122535A Pending CN1784236A (zh) 2003-05-07 2004-05-03 雄激素受体调节剂及其使用方法

Country Status (7)

Country Link
US (2) US7351698B2 (enExample)
EP (1) EP1622567B1 (enExample)
JP (1) JP4832303B2 (enExample)
CN (1) CN1784236A (enExample)
AU (1) AU2004238238C1 (enExample)
CA (1) CA2524409C (enExample)
WO (1) WO2004100874A2 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103694299A (zh) * 2014-01-13 2014-04-02 中国药科大学 甾体类雄激素受体抑制剂、其制备方法及其医药用途
CN108727453A (zh) * 2017-04-20 2018-11-02 华东理工大学 新型pd-1抑制剂及其应用

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2012014431A (es) 2010-06-10 2013-02-26 Aragon Pharmaceuticals Inc Modulares del receptor de estrogenos y usos de los mismos.
MX357496B (es) 2011-12-14 2018-07-11 Seragon Pharmaceuticals Inc Moduladores del receptor de estrógenos fluorados y sus usos.
NZ710707A (en) 2013-02-08 2016-10-28 Footfalls And Heartbeats Ltd Method for optimizing contact resistance in electrically conductive textiles
CN103445892A (zh) * 2013-08-02 2013-12-18 苏州市马尔泰新材料有限公司 一种含有甲酯树脂和雌酚的阴道模具
CN103394127A (zh) * 2013-08-02 2013-11-20 苏州市马尔泰新材料有限公司 一种含有中西医药的阴道模具材料
CN103431930A (zh) * 2013-08-02 2013-12-11 苏州市马尔泰新材料有限公司 一种含有甲酯树脂的阴道模具
CN103405810A (zh) * 2013-08-02 2013-11-27 苏州市马尔泰新材料有限公司 一种含有甲基丙烯酸甲酯树脂的阴道模具
CN103394128A (zh) * 2013-08-02 2013-11-20 苏州市马尔泰新材料有限公司 一种含有川芎的模具材料
CN103393489A (zh) * 2013-08-02 2013-11-20 苏州市马尔泰新材料有限公司 一种含有雌二醇的阴道模具
EP3033448A1 (en) 2013-08-16 2016-06-22 Footfalls and Heartbeats Limited Method for making electrically conductive textiles and textile sensor
JP2020502218A (ja) 2016-12-21 2020-01-23 メレオ バイオファーマ ３ リミテッド 骨形成不全症の処置における抗スクレロスチン抗体の使用
PT3691620T (pt) 2017-10-05 2022-10-06 Fulcrum Therapeutics Inc Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD

Family Cites Families (16)

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US4377584A (en) * 1978-04-13 1983-03-22 Merck & Co., Inc. 4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
IE76452B1 (en) * 1990-10-29 1997-10-22 Sankyo Co Azasteroid compounds for the treatment of prostatic hypertrophy their preparation and use
US5710275A (en) * 1992-05-20 1998-01-20 Merck & Co., Inc. 7β-substituted-4-aza-5α-androstan-3-ones as 5α-reductase inhibitors
AU4251993A (en) * 1992-05-20 1993-12-13 Merck & Co., Inc. Substituted 4-aza-5A-androstan-ones as 5A-reductase inhibitors
WO1993023038A1 (en) * 1992-05-20 1993-11-25 Merck & Co., Inc. 17-AMINO SUBSTITUTED 4-AZASTEROID 5α-REDUCTASE INHIBITORS
ES2149208T3 (es) * 1992-05-20 2000-11-01 Merck & Co Inc Inhibidores 4-azaesteroides de 5-alfa-reductasa.
AU4258493A (en) * 1992-05-21 1993-12-13 Endorecherche Inc. Inhibitors of testosterone 5alpha-reductase activity
HU212459B (en) * 1992-10-02 1996-06-28 Richter Gedeon Vegyeszet Process for producing new 17-beta-substituted 4-aza-androstane-derivatives and pharmaceutical compositions containing them
DE69329933T2 (de) * 1992-10-06 2001-07-19 Merck & Co., Inc. 17-beta-carboxanilid derivate von 4-aza-5-alpha-androstan-3-one als 5-alpha-reduktase-hemmende arzneimittel
US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
ATE215093T1 (de) * 1993-06-24 2002-04-15 Richter Gedeon Vegyeszet 17-halogen-4-azaandrosten-derivate und verfahren zu ihrer herstellung
AU681585B2 (en) 1993-06-24 1997-09-04 Richter Gedeon Vegyeszeti Gyar Rt. Novel process for preparing 17beta -substituted 4-azaandrostane derivatives
US6001844A (en) * 1995-09-15 1999-12-14 Merck & Co., Inc. 4-Azasteroids for treatment of hyperandrogenic conditions
AU713582B2 (en) * 1995-10-26 1999-12-02 Merck & Co., Inc. 4-oxa and 4-thia steroids
EP0880540B1 (en) 1996-02-14 2002-06-12 Aventis Pharmaceuticals Inc. 17-beta-cyclopropyl(amino/oxy) 4-aza steroids as active inhibitors of testosterone 5-alpha-reductase and c17-20-lyase
AU5791698A (en) * 1996-12-09 1998-07-03 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103694299A (zh) * 2014-01-13 2014-04-02 中国药科大学 甾体类雄激素受体抑制剂、其制备方法及其医药用途
CN108727453A (zh) * 2017-04-20 2018-11-02 华东理工大学 新型pd-1抑制剂及其应用

Also Published As

Publication number Publication date
EP1622567B1 (en) 2013-07-24
AU2004238238A1 (en) 2004-11-25
CA2524409A1 (en) 2004-11-25
JP2006528686A (ja) 2006-12-21
US20080119503A1 (en) 2008-05-22
US7351698B2 (en) 2008-04-01
CA2524409C (en) 2011-12-20
AU2004238238B2 (en) 2009-07-16
EP1622567A2 (en) 2006-02-08
JP4832303B2 (ja) 2011-12-07
US20060241107A1 (en) 2006-10-26
EP1622567A4 (en) 2009-04-29
WO2004100874A3 (en) 2006-01-26
WO2004100874A2 (en) 2004-11-25
AU2004238238C1 (en) 2010-01-14

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Open date: 20060607